Cholesterylbutyrate solid lipid nanoparticles as a butyric acid prodrug

Molecules. 2008 Feb 1;13(2):230-54. doi: 10.3390/molecules13020230.


Cholesterylbutyrate (Chol-but) was chosen as a prodrug of butyric acid. Butyrate is not often used in vivo because its half-life is very short and therefore too large amounts of the drug would be necessary for its efficacy. In the last few years butyric acid's anti-inflammatory properties and its inhibitory activity towards histone deacetylases have been widely studied, mainly in vitro. Solid Lipid Nanoparticles (SLNs), whose lipid matrix is Chol-but, were prepared to evaluate the delivery system of Chol-but as a prodrug and to test its efficacy in vitro and in vivo. Chol-but SLNs were prepared using the microemulsion method; their average diameter is on the order of 100-150 nm and their shape is spherical. The antineoplastic effects of Chol-but SLNs were assessed in vitro on different cancer cell lines and in vivo on a rat intracerebral glioma model. The anti-inflammatory activity was evaluated on adhesion of polymorphonuclear cells to vascular endothelial cells. In the review we will present data on Chol-but SLNs in vitro and in vivo experiments, discussing the possible utilisation of nanoparticles for the delivery of prodrugs for neoplastic and chronic inflammatory diseases.

Publication types

  • Review

MeSH terms

  • Animals
  • Cell Death / drug effects
  • Cholesterol Esters / chemistry*
  • Cholesterol Esters / pharmacology*
  • Humans
  • Lipids / chemistry*
  • Lipids / pharmacology
  • Nanoparticles / chemistry*
  • Prodrugs / chemistry*
  • Prodrugs / pharmacology


  • Cholesterol Esters
  • Lipids
  • Prodrugs
  • cholesteryl butanoate